Process for producing an injectable medicament preparation

Abstract

The invention relates to a method for producing injectable medicament preparations containing a therapeutically and/or diagnostically effective substance which is comprised of an active agent, of a spacer molecule and of at least one protein-binding molecule. After being brought into contact with the body, said therapeutically and/or diagnostically effective substance covalently bonds to the body fluid constituents or tissue constituents via the protein-binding molecule, thus providing a form of transport of the active agent that an be hydrolytically or enzymatically cleaved, according to pH, in the body while releasing the active agent.

1 - 19 . (canceled)  
     
     
         20 . A therapeutically or diagnostically effective substance comprising at least one active compound selected from the group consisting of cytostatic agent, a cytokine, an immunosuppressive agent, a virostatic agent, an antirheumatic agent, an analgesic, an antiinflammatory agent, an antibiotic, an antimicotic agent, a signal transduction inhibitor, an angiogenesis inhibitor or a protease inhibitor, at least one protein-binding molecular residue selected from the group consisting of maleimide, haloacetamide, haloacetate, pyridylthio, N-hydroxysuccinimide ester, isothiocyanate, disulphide, vinylcarbonyl, aziridine and acetylene which is linked to the active compound through a spacer comprising an organic molecular residue, which contains at least one aliphatic carbon chain, or an aliphatic carbon ring having 1-12 carbon atoms, some of which can be replaced with oxygen, or at least one aromatic moiety, with the spacer, or the bond between the spacer and the active compound, being cleavable hydrolytically or enzymatically in the body in a pH-dependent manner, and whereas the active compound is not a cytostatic agent.  
     
     
         21 . The compound of formula  
       
         
           
           
               
               
           
         
       
     
     
         22 . A method for treating cancer diseases, virus diseases, autoimmune diseases, acute or chronic inflammatory diseases and diseases which are caused by bacteria, fungi or other microorganisms comprising administering the therapeutically or diagnostically effective substance of  claim 20  to a patient.  
     
     
         23 . A diagnostic kit comprising a protein-binding diagnostically effective substance according to  claim 20 , pharmaceutically acceptable auxiliary, substance, a carrier or a diluent.  
     
     
         24 . A method for detecting cancer diseases, auto immune diseases, acute or chronic inflammatory diseases and diseases which are caused by viruses or microorganisms, or for detecting the carrier molecule and its distribution in the body comprising utilizing the kit of  claim 23 .  
     
     
         25 . A process for producing an injectable medicament preparation, which comprises a diagnostically effective substance which is dissolved in an injectable carrier liquid, wherein the diagnostically effective substance comprises a diagnostic agent selected from the group consisting of a radionuclide, a positron emitters, a NMR contrast agent, a fluorescent compound and a contrast agent in the near IR range, a spacer comprising an organic molecular residue, which contains at least one aliphatic carbon chain, or an aliphatic carbon ring having 1-12 carbon atoms, some of which can be replaced with oxygen, or at least one aromatic moiety, and at least one protein-binding molecular residue selected from the group consisting of maleimide, haloacetamide, haloacetate, pyridylthio, N-hydroxysuccinimide ester, isothiocyanate, disulphide, vinylcarbonyl, aziridine and acetylene.  
     
     
         26 . A process according to  claim 25 , wherein said spacer is phenylacetylhydrazone.  
     
     
         27 . A process according to  claim 25  wherein the bond between the diagnostic agent and the protein-binding molecular residue or the spacer is not cleavable.  
     
     
         28 . A method according to  claim 22  wherein the disease is cancer and the compound is  
       
         
           
           
               
               
           
         
       
     
     
         29 . The compound of the formula  
       
         
           
           
               
               
           
         
       
     
     
         30 . A method according to  claim 22  wherein the disease is cancer and the compound is  
       
         
           
           
               
               
           
         
       
     
     
         31 . The method of  claim 22 , wherein the compound is